synthesis and anticonvulsant activity evaluation of 3-alkoxy-4-(4- (hexyloxy/heptyloxy)phenyl)-4h-1,2,4 -triazole

نویسندگان

yingquan fang ollege of pharmacy, yanbian university and department of pharmacy,chongqing three gorges medical college

chunling sun college of pharmacy, yanbian university

dachuan liu college of pharmacy, yanbian university

shiben wang college of pharmacy, yanbian university

چکیده

a series of 3-alkoxy-4-(4-(hexyloxy/heptyloxy) phenyl)-4h-1,2,4-triazole was synthesized. the anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (mes) test and rotarod tests with intraperitoneally injected mice. among the synthesized compounds, compound 3-heptyloxy-4-(4-(hexyloxy) phenyl)-4h-1,2,4-triazole (5f) was the most active one and also had the lowest toxicity. in the anti-mes potency test, it showed median effective dose (ed50) of 37.3mg/kg, median toxicity dose (td50) of 422.5 mg/kg, and the protective index (pi) of 11.3 which is much greater than the reference drug carbamazepine with pi value of 6.4. as well as demonstrating the anti-mes efficacy of compound 5f, its potency against seizures induced by pentylenetetrazole, 3-mercaptopropionic acid, and bicuculline were also established, with the results suggesting that gaba-mediated mechanisms might be involved in its anticonvulsant activity, such as enhancing of gabaergic neurotransmission or activity, activate gad or inhibit gaba-t, and gabaa-mediated mechanisms.

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Synthesis and Anticonvulsant Activity Evaluation of 3-alkoxy-4-(4- (hexyloxy/heptyloxy)phenyl)-4H-1,2,4 -triazole

A series of 3-alkoxy-4-(4-(hexyloxy/heptyloxy) phenyl)-4H-1,2,4-triazole was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test and rotarod tests with intraperitoneally injected mice. Among the synthesized compounds, compound 3-heptyloxy-4-(4-(hexyloxy) phenyl)-4H-1,2,4-triazole (5f) was the most active one and also had...

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Synthesis and Anticonvulsant Activity Evaluation of 3-alkoxy-4-(4- (hexyloxy/heptyloxy)phenyl)-4H-1,2,4 -triazole

A series of 3-alkoxy-4-(4-(hexyloxy/heptyloxy) phenyl)-4H-1,2,4-triazole was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test and rotarod tests with intraperitoneally injected mice. Among the synthesized compounds, compound 3-heptyloxy-4-(4-(hexyloxy) phenyl)-4H-1,2,4-triazole (5f) was the most active one and also had...

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Synthesis and Anticonvulsant Activity Evaluation of 3-alkoxy-4-(4-(hexyloxy/heptyloxy)phenyl)-4H-1,2,4 -triazole

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عنوان ژورنال:
iranian journal of pharmaceutical research

جلد ۱۴، شماره ۱، صفحات ۷۷-۸۷

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